NO20100004L - Hepatitt C inhibitor tripeptider - Google Patents

Hepatitt C inhibitor tripeptider

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Publication number
NO20100004L
NO20100004L NO20100004A NO20100004A NO20100004L NO 20100004 L NO20100004 L NO 20100004L NO 20100004 A NO20100004 A NO 20100004A NO 20100004 A NO20100004 A NO 20100004A NO 20100004 L NO20100004 L NO 20100004L
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NO
Norway
Prior art keywords
alkyl
het
optionally substituted
formula
lower alkyl
Prior art date
Application number
NO20100004A
Other languages
English (en)
Other versions
NO336663B1 (no
Inventor
Montse Llinas-Brunet
Murray D Bailey
Dale Cameron
Anne-Marie Faucher
Elise Ghiro
Nathalie Goudreau
Teddy Halmos
Marc-Andre Poupart
Jean Rancourt
Youla S Tsantrizos
Dominik M Wernic
Original Assignee
Boehringer Ingelheim Ca Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Publication of NO20100004L publication Critical patent/NO20100004L/no
Application filed by Boehringer Ingelheim Ca Ltd filed Critical Boehringer Ingelheim Ca Ltd
Publication of NO336663B1 publication Critical patent/NO336663B1/no

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    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P13/00Preparation of nitrogen-containing organic compounds
    • C12P13/02Amides, e.g. chloramphenicol or polyamides; Imides or polyimides; Urethanes, i.e. compounds comprising N-C=O structural element or polyurethanes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P41/00Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
    • C12P41/003Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions
    • C12P41/005Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions by esterification of carboxylic acid groups in the enantiomers or the inverse reaction

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Analytical Chemistry (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Racemater, diastereoisomerer og optiske isomerer av en forbindelse av formel (I) hvor B er H, en C6 eller C10 aryl, C7-16 aralkyl; Het eller (lavere alkyl)-Het, hvorav alle eventuelt er substituert med C1-6alkyl; C1-6alkoksy; C1-6alkanoyl; hydroksy; hydroksy alkyl; halogen; halogenalkyl; nitro; cyano; cyanoalkyl; amino eventuelt substituert med C1-6alkyl; amido; eller (lavere alkyl)amid; eller B er et acylderivat av formel R4-C(O)-; en karboksyl av formel R4-O-C(O)-; et amid av formel R4-N(R5)-C(O)-; et tioamid av formel R4-N(R5)-C(S)-; eller et sulfonyl av formel R4 SO2; R5 er H eller C1-6alkyl; og Y er H eller C1-6alkyl; R3 er C1-8alkyl, C3-7cykloalkyl eller C4-ioalkylcykloalkyl, alle eventuelt substituert med hydroksy, d-6alkoksy, C1- etioalkyl, amido, (lavere alkyl)amido, C6 eller Ci0aryl, eller C7-i6aralkyl; R2 er CH2-R20, NH-R20, O-R20 eller S- R20, hvori R20 er en mettet eller umettet C3-7cykloalkyl eller C4-io(alkylcykloalkyl), hvorav alle er eventuelt mono-, di- eller tri-substituert med R2i, eller R20 er en C6 eller Ci0aryl eller C7-i4aralkyl, eventuelt substituert, eller R20 er Het eller (lavere alkyl)-Het, begge eventuelt substituert, Het eller (lavere alkyl)-Het; karboksyl; karboksy(lavere alkyl); C6 eller d0aryl, C7. i4aralkyl eller Het, idet nevnte aryl, aralkyl eller Het er eventuelt substituert; og R1 er H; C1-6alkyl, C3- 7cykloalkyl, C2-6alkenyl, eller C2-6alkynyl, alle eventuelt substituert med halogen; eller et farmasøytisk akseptabelt salt eller en ester derav.
NO20100004A 1998-08-10 2010-01-05 Fremgangsmåte for oppløsning av en enantiomer blanding av 1-amino-2-vinylcyclopropyl karboksylsyrederivater NO336663B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US9593198P 1998-08-10 1998-08-10
US13238699P 1999-05-04 1999-05-04
PCT/CA1999/000736 WO2000009543A2 (en) 1998-08-10 1999-08-09 Hepatitis c inhibitor tri-peptides

Publications (2)

Publication Number Publication Date
NO20100004L true NO20100004L (no) 2001-04-02
NO336663B1 NO336663B1 (no) 2015-10-12

Family

ID=26790767

Family Applications (2)

Application Number Title Priority Date Filing Date
NO20010683A NO328952B1 (no) 1998-08-10 2001-02-09 Tripeptidforbindelser, fremgangsmate for fremstilling av disse, farmasoytisk preparat, anvendelse av forbindelsene for fremstilling av et medikament for behandling av sykdom.
NO20100004A NO336663B1 (no) 1998-08-10 2010-01-05 Fremgangsmåte for oppløsning av en enantiomer blanding av 1-amino-2-vinylcyclopropyl karboksylsyrederivater

Family Applications Before (1)

Application Number Title Priority Date Filing Date
NO20010683A NO328952B1 (no) 1998-08-10 2001-02-09 Tripeptidforbindelser, fremgangsmate for fremstilling av disse, farmasoytisk preparat, anvendelse av forbindelsene for fremstilling av et medikament for behandling av sykdom.

Country Status (43)

Country Link
US (11) US6323180B1 (no)
EP (2) EP2028186B1 (no)
JP (2) JP4485685B2 (no)
KR (2) KR100672229B1 (no)
CN (2) CN100339389C (no)
AR (3) AR020880A1 (no)
AT (1) ATE430158T1 (no)
AU (1) AU769738B2 (no)
BG (1) BG65738B1 (no)
BR (2) BR9917805B1 (no)
CA (2) CA2445938C (no)
CO (1) CO5261542A1 (no)
CY (2) CY1109291T1 (no)
CZ (2) CZ302766B6 (no)
DE (1) DE69940817D1 (no)
DK (2) DK1105413T3 (no)
EA (1) EA003906B1 (no)
EE (1) EE05517B1 (no)
ES (2) ES2405930T3 (no)
HK (2) HK1040085B (no)
HR (1) HRP20010102B1 (no)
HU (2) HU229262B1 (no)
ID (1) ID27839A (no)
IL (3) IL141012A0 (no)
IN (3) IN211493B (no)
ME (1) ME00381B (no)
MX (2) MX261584B (no)
MY (1) MY127538A (no)
NO (2) NO328952B1 (no)
NZ (1) NZ510396A (no)
PE (1) PE20000949A1 (no)
PH (1) PH11999002002B1 (no)
PL (1) PL204850B1 (no)
PT (2) PT1105413E (no)
RS (3) RS53562B1 (no)
SA (1) SA99200617B1 (no)
SI (2) SI1105413T1 (no)
SK (2) SK288068B6 (no)
TR (2) TR200200129T2 (no)
TW (1) TWI250165B (no)
UA (1) UA75026C2 (no)
WO (1) WO2000009543A2 (no)
ZA (1) ZA200100971B (no)

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